佐芬普利
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- CAS号:
- 81872-10-8
- 英文名:
- Zofenopril
- 英文别名:
- NAA;NAA(R);NAA(TM);ALPHA-NAA;Zofenopril;ROOTONE(R);FRUIT FAX(R);Zofenopril-d5;AKOS AU36-M588;RARECHEM AL BO 0198
- 中文名:
- 佐芬普利
- 中文别名:
- 佐芬普利;佐芬普利;佐芬普利杂质;佐芬普利-D5;硝酸萘甲唑啉杂质B;化合物 ZOFENOPRIL;4S-1-[D-3-(苯甲酰硫基)-2-甲基丙酰]-4-(苯硫基)-L-脯氨酸
- CBNumber:
- CB1679843
- 分子式:
- C22H23NO4S2
- 分子量:
- 429.55
- MOL File:
- 81872-10-8.mol
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佐芬普利化学性质
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熔点:
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129-131.5 °C(lit.)
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比旋光度:
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D25 -36.5° (c = 1 in methanol)
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沸点:
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646.3±55.0 °C(Predicted)
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密度:
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1.34±0.1 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO: 5 mg/mL (11.64 mM)
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形态:
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crystalline
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酸度系数(pKa):
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pK1:4.236 (25°C)
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颜色:
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light yellow
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CAS 数据库:
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81872-10-8(CAS DataBase Reference)
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佐芬普利性质、用途与生产工艺
佐芬普利为首个含有巯基的长效ACE抑制剂，由于其含有巯基，因此使之具有亲脂性和抗氧化特性，本品可水解为活性物佐芬普利拉。
佐芬普利用于轻至中度原发性高血压治疗，以及用于急性心肌梗死24小时内有或无症状、血流动力学稳定并未接受溶栓治疗的患者。
佐芬普利常见不良反应为有头晕（3.9％）、疲劳（2.6％）、头痛（2.4％）、咳嗽（1.2％）、恶心或呕吐（1.2％）。
不常见的不良瓜为潮红（0.8％）、肌痉挛（0.8％）和虚弱（0.5％）。
Zofenopril 是一个 angiotensin-converting enzyme (ACE) 抑制剂，其 IC50 值为 81 μM。
Kinetic analyses demonstrate that enalapril inhibits the uptake of GlySar in a competitive manner (K
i
approximately 6 mM). Fosinopril and Zofenopril have the greatest inhibitory potency (IC
50
values of 55 and 81μM, respectively) while the other ACE inhibitors exhibit low-affinity interactions with the renal peptide transporter.
Zofenopril, a sulphydrylic compound, at doses higher than 70 mg/kg i.p. produces significant protection (i.e. at 70 mg/kg, P=0.044, F=2.17, d.f.=18; at higher concentration P<0.05) against the tonic phase of the audiogenic seizure response. Pretreatment with Zofenopril (15 mg/kg, i.p.) is able to produce a consistent shift to the left of the dose-response curves and a significant reduction of ED
50
values against clonus of some AEDs with the exceptions of diazepam, felbamate, phenobarbital and phenytoin compare with concurrent groups, suggesting an increase in anticonvulsant activity.
佐芬普利
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/08/19 | HY-108321S | Zofenopril-d5 | | 1 mg | 2350元 |
| 2024/08/19 | HY-108321 | 1-萘乙酸
Zofenopril | 81872-10-8 | 5mg | 1600元 |
佐芬普利
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81872-10-8, 佐芬普利 相关搜索:
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- 化合物 ZOFENOPRIL
- 4S-1-[D-3-(苯甲酰硫基)-2-甲基丙酰]-4-(苯硫基)-L-脯氨酸
- 佐芬普利杂质
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- 佐芬普利-D5
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- (naphthalen-1-yl)acetic acid (1-naphthylacetic acid)
- Zofenopril D5Q: What is
Zofenopril D5 Q: What is the CAS Number of
Zofenopril D5 Q: What is the storage condition of
Zofenopril D5 Q: What are the applications of
Zofenopril D5
- Zofenopril-d5 USP/EP/BP
- L-Proline, 1-[(2S)-3-(benzoylthio)-2-methyl-1-oxopropyl]-4-(phenylthio)-, (4S)-
- (2S,4S)-1-[(2S)-3-(benzoylthio)-2-methyl-1-oxopropyl]-4-(phenylthio)-2-pyrrolidinecarboxylic acid
- AKOS AU36-M588
- ALPHA-NAA
- FRUIT FAX(R)
- Zofenopril-d5
- (2S,4S)-1-[(2S)-3-(benzoylthio)-2-methyl-propanoyl]-4-(phenylthio)proline
- (2S,4S)-1-[(2S)-3-(benzoylsulfanyl)-2-methylpropanoyl]-4-phenylsulfanylpyrrolidine-2-carboxylic acid
- (2S,4S)-1-[(2S)-2-methyl-3-phenylcarbonylsulfanyl-propanoyl]-4-phenylsulfanyl-pyrrolidine-2-carboxylic acid
- ROOTONE(R)
- RARECHEM AL BO 0198
- NAPHTHALENEACETIC ACID
- NAA
- NAA(TM)
- NAA(R)
- Zofenopril
- (4S)-N-[3-(Benzoylsulfanyl)-2(S)-methylpropionyl]-4-(phenylsulfanyl)-L-proline
- S-Benzoyl-4-phenylthiocaptopril
- 1-[(S)-3-(Benzoylthio)-2-methyl-1-oxopropyl]-4α-(phenylthio)-L-proline
- 1-NAPHTHYLACETICACIDα-NAPHTHYLACETICACID